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Issue 5, 2017
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2-Arylaminobenzothiazole-arylpropenone conjugates as tubulin polymerization inhibitors

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Abstract

A new series of 2-arylaminobenzothiazole-arylpropenone conjugates 56(ar) was designed, synthesized and investigated for their cytotoxic potency against the various human cancer cell lines. Most of these conjugates exhibited cytotoxic activity and inhibited in vitro tubulin polymerization effectively. Conjugates 5d and 6d cause cell cycle blocks in the G2/M phase in HeLa cells and treatments with 5d and 6d manifested increased mRNA and protein levels of the G2/M marker, cyclin B1. Immunocytochemistry revealed loss of intact microtubule structure in cells treated with 5d and 6d. Western blot analysis revealed that these conjugates accumulate more tubulin in the soluble fraction. Moreover, the triggering of apoptotic cell death after mitotic arrest was investigated by studying their effect on Hoechst staining, mitochondrial membrane potential, ROS generation.

Graphical abstract: 2-Arylaminobenzothiazole-arylpropenone conjugates as tubulin polymerization inhibitors

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Publication details

The article was received on 11 Oct 2016, accepted on 05 Jan 2017 and first published on 07 Mar 2017


Article type: Research Article
DOI: 10.1039/C6MD00562D
Citation: Med. Chem. Commun., 2017,8, 924-941
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    2-Arylaminobenzothiazole-arylpropenone conjugates as tubulin polymerization inhibitors

    A. V. Subba Rao, B. B. Rao, S. Sunkari, S. P. Shaik, B. Shaik and A. Kamal, Med. Chem. Commun., 2017, 8, 924
    DOI: 10.1039/C6MD00562D

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